盐酸伐昔洛韦泡腾片在人体内的生物等效性

Relative bioavailability of Valaciclovir hydrochloride effervescent tablets in healthy volunteers

目的考察两种盐酸伐昔洛韦片的人体生物等效性。方法采用双制剂双周期自身交叉对照的方法,将18名健康男性受试者随机分为两组,单剂量口服盐酸伐昔洛韦受试制剂和参比制剂各0.6 g;血浆中阿昔洛韦浓度用HPLC法测定,DAS软件计算药物动力学参数,并对其进行生物等效性评价。结果盐酸伐昔洛韦受试制剂和参比制剂的Cm ax分别为2.54±0.32、2.59±0.44μg.m l-1;Tm ax分别为2.28±0.31、2.22±0.26 h;AUC0→Tn分别为10.75±1.804、11.35±2.548μg.h.m l-1,AUC0→∞分别为11.49±2.06、12.09±2.757μg.h.m l-1;t1/2分别为2.55±0.69 h、2.67±0.76 h。按盐酸伐昔洛韦药-时曲线下0→Tn的面积计算,相对生物利用度为96.1%。结论盐酸伐昔洛韦受试制剂与参比制剂相比,AUC、Cm ax符合生物等效性要求,Tm ax比较差异无统计学意义,受试制剂和参比制剂具有生物等效性。

OBJECTIVE To investigate the relative bioavailability of two kinds of Valaciclovir hydrochloride effervescent tablet in healthy volunteers. METHODS According to a paired,cross - over design, 18 healthy male volunteers were randomly divided into two groups. A single oral dose of 0.6 g Valaciclovir hydrochloride, either the test effervescent or its reference was given to them. The plasma concentration of Acyclovir was determined by HPLC with ultraviolet detection. The pharmacokinetic parameters were calculated by DAS program and the bioequivalence of the two tablets was evaluated. RESULTS For test and reference preparations, Cmax were 2.54 ± 0.32 μg·ml^-1 and 2.59 ±0.44 μg·ml^-1, Tmax, were 2.28 ±0.31 h and 2.22 ±0.26 h, AUC0→Tn were 10.75 ±1. 804 μg·h·ml ^-1 and 11.35±2.548 μg·h·ml^-1 ,AUC0→∞ were 11.49 ±2.06 μg·h·ml^-1 and 12.09±2.757 μg ·h·ml^-1, t1/2 were 2.55±0.69 h and 2. 67±0.76 h, respectively. The relative bioavailability of the test was 96.1%. CONCLUSION The test preparation of Valaciclovir hydroehlodde effervescent tablets are bioequivalent to the reference preparation.